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US 5,348,966 AGranted
Method for treating pyoderma and Sezary's syndrome using FK 506 and related compounds
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsThomas E. Starzl, Satoru Todo
Life of this patent
Estimating the term…
Abstract
Administration of FK506 or related macrolide compounds is effective for the treatment of pyoderma and Sezary's syndrome.
Claims15
A method for treating pyoderma, comprising administering, to a patient in need thereof, an effective amount of a compound of the formula (I) ##STR3## wherein each vicinal pair of substituents (R.sup.1 and R.sup.2), (R.sup.3 and R.sup.4), (R.sup.5 and R.sup.6) independently
- a) represent two vicinal hydrogen atoms, or
- b) form a second bond between the vicinal carbon atoms to which they are attached;
- in addition to its significance above, R.sup.2 may represent an alkyl group;
- R.sup.7 represents H, OH, protected hydroxy or O-alkyl, or in conjunction with R.sup.1 it may represent .dbd.O;
- R.sup.8 and R.sup.9 independently represent H or OH;
- R.sup.10 represents H, alkyl, alkyl substituted by one or more hydroxyl groups, alkenyl, alkenyl substituted by one or more hydroxyl groups, or alkyl substituted by .dbd.O;
- X represents O, (H,OH), (H,H) or --CH.sub.2 O--;
- Y represents O, (H,OH), (H,H), N--NR.sup.11 R.sup.12 or N--OR.sup.13 ;
- R.sup.11 and R.sup.12 independently represent H, alkyl, aryl or tosyl;
- R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.22 and R.sup.23 independently represent H or alkyl;
- R.sup.20 and R.sup.21 independently represent O, or they may independently represent (R.sup.20 a,H) and (R.sup.21 a,H) respectively;
- R.sup.20 a and R.sup.21 a independently represent OH, O-alkyl or OCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 or R.sup.21 a is protected hydroxy;
- in addition, R.sup.20 a and R.sup.21 a may together represent an oxygen atom in an epoxide ring;
- n is 1, 2 or 3;
- in addition to their significances above, Y, R.sup.10 and R.sup.23, together with the carbon atoms to which they are attached, may represent a 5- or 6- membered N-, S- or O- containing heterocyclic ring, which may be saturated or unsaturated, and which may be substituted by one or more groups selected from alkyl, hydroxy, alkyl substituted by one or more hydroxyl groups, O-alkyl, benzyl and --CH.sub.2 Se(C.sub.6 H.sub.5);
- and pharmaceutically acceptable salts thereof.
13 more elements
A method for treating Sezary's syndrome, comprising administering, to a patient in need thereof, an effective amount of a compound of formula (I) ##STR4## wherein each vicinal pair of substituents (R.sup.1 and R.sup.2), (R.sup.3 and R.sup.4), (R.sup.5 and R.sup.6) independently
- a) represent two vicinal hydrogen atoms, or
- b) form a second bond between the vicinal carbon atoms to which they are attached;
- in addition to its significance above, R.sup.2 may represent an alkyl group;
- R.sup.7 represents H, OH, protected hydroxy or O-alkyl, or in conjunction with R.sup.1 it may represent .dbd.O;
- R.sup.8 and R.sup.9 independently represent H or OH;
- R.sup.10 represents H, alkyl, alkyl substituted by one or more hydroxyl groups, alkenyl, alkenyl substituted by one or more hydroxyl groups, or alkyl substituted by .dbd.O;
- X represents O, (H,OH), (H,H) or --CH.sub.2 O--;
- Y represents O, (H,OH), (H,H), or N--NR.sup.11 R.sup.12 or N--OR.sup.13 ;
- R.sup.11 and R.sup.12 independently represent H, alkyl, aryl or tosyl;
- R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.22 and R.sup.23 independently represent H or alkyl;
- R.sup.20 and R.sup.21 independently represent O, or they may independently represent (R.sup.20 a,H) and (R.sup.21 a,H) respectively;
- R.sup.20 a and R.sup.21 a independently represent OH, O-alkyl or OCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 or R.sup.21 a is protected hydroxy;
- in addition, R.sup.20 a and R.sup.21 a may together represent an oxygen atom in an epoxide ring;
- n is 1, 2 or 3;
- in addition to their significances above, Y, R.sup.10 and R.sup.23, together with the carbon atoms to which they are attached, may represent a 5- or 6- membered N-, S- or O- containing heterocyclic ring, which may be saturated or unsaturated, and which may be substituted by one or more groups selected from alkyl, hydroxy, alkyl substituted by one or more hydroxyl groups, O-alkyl, benzyl and --CH.sub.2 Se(C.sub.6 H.sub.5);
- and pharmaceutically acceptable salts thereof.
13 more elements
Dependencies are inferred from the claim text.